1-benzyloxynaphthalene-2-carboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-benzyloxynaphthalene-2-carboxylic acid
• 英文别名: 1-benzyloxy-2-naphthoic acid；1-benzyloxy-naphthalene-2-carboxylic acid；1-(Benzyloxy)-2-naphthoic acid；1-phenylmethoxynaphthalene-2-carboxylic acid
• 化学式: C₁₈H₁₄O₃
• mdl: MFCD18262675
• 分子量: 278.307
• InChiKey: QIZFUOOPZJHIFV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.055
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-benzyloxynaphthalene-2-carboxylic acid 在 palladium 10% on activated carbon 、 氢气 、 4-甲基苯磺酸吡啶 作用下， 以 四氢呋喃 、 乙酸乙酯 、 间二甲苯 为溶剂， 20.0 ℃ 、206.85 kPa 条件下， 反应 29.0h， 生成 2-(1-hydroxy-naphthalen-2-yl)benzoxazole-4-carboxylic acid methyl ester
  参考文献：
  名称：

  UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication

  摘要：

  The bacterial natural product UK-1 and several structural analogs inhibit replication of the hepatitis C virus in the replicon assay, with IC50 values as low as 0.50 mu M. The NS3 helicase has been identified as a possible target of inhibition for several of these compounds, while the remaining inhibitors act via an undetermined mechanism. Gel shift assays suggest that helicase inhibition is a direct result of inhibitor-enzyme binding as opposed to direct RNA binding, and the ATPase activity of NS3 is not affected. The syntheses and biological results are presented herein. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.12.012
• 作为产物：
  描述：

  1-羟基-2-萘甲酸 在 四丁基溴化铵 、 potassium carbonate 、 sodium hydroxide 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 1-benzyloxynaphthalene-2-carboxylic acid
  参考文献：
  名称：

  含PO分子的扩环反应

  摘要：

  一系列含PO分子的扩环反应已被开发用于合成中等大小环的环状膦酸酯和膦酰胺酯。与更完善的内酰胺衍生物扩环反应相比，反应性趋势最初似乎是反直觉的，但可以通过考虑分别与 P 和 C 杂原子键合的差异来解释。

  DOI：

  10.1039/d3cc02087h

文献信息

• [EN] 2-NAPHTAMIDE DERIVATIVES<br/>[FR] DERIVES DE 2-NAPHTAMIDE
  申请人：BAYER AG

  公开号：WO2003106402A1

  公开（公告）日：2003-12-24

  The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.

  本发明涉及2-萘酰胺，其作为药物制剂的有效成分。本发明的2-萘酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。这些疾病包括泌尿系统疾病或障碍，如：膀胱出口梗阻、膀胱过度活跃、尿失禁、膀胱逼尿肌超反射、膀胱逼尿肌不稳定、膀胱容量降低、排尿频率增加、急迫性尿失禁、压力性尿失禁、膀胱高反应性、良性前列腺肥大（BPH）、前列腺炎、尿频、夜尿频、尿急、盆腔过敏、尿道炎、盆腔疼痛综合征、前列腺疼痛综合征、膀胱炎或特发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛、神经病性疼痛、急性疼痛、慢性疼痛、牙痛、经前疼痛、内脏疼痛、头痛等；低血压；血友病和出血；以及炎症，因为通过IP受体拮抗剂治疗也能缓解该疾病。
• Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compouds
  申请人：Zhou Yuefen

  公开号：US20050239827A1

  公开（公告）日：2005-10-27

  The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammals, especially humans.

  本发明涉及抗菌3,5-二氨基哌啶取代的芳香族和杂环化合物及其制药组合物。本发明还涉及一种使用这些化合物治疗哺乳动物（尤其是人类）细菌感染的方法。
• 2-naphthamide derivatives
  申请人：Shimazaki Makoto

  公开号：US20060166989A1

  公开（公告）日：2006-07-27

  The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), pro-statitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.

  本发明涉及2-萘酰胺，其作为药物制剂的活性成分具有重要用途。本发明的2-萘酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。此类疾病包括以下泌尿系统疾病或障碍：膀胱出口梗阻、过度活跃的膀胱、尿失禁、膀胱平滑肌过度反射、膀胱平滑肌不稳定性、膀胱容量减少、排尿频率、切实尿失禁、压力性尿失禁、膀胱过度反应、前列腺增生症（BPH）、前列腺炎、尿频、夜尿、尿急、盆腔过敏、尿道炎、盆腔疼痛综合征、前列腺痛、膀胱炎或特发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛、神经病理性疼痛、急性疼痛、慢性疼痛、牙痛、经前期疼痛、内脏疼痛、头痛等；低血压；血友病和出血；以及炎症，因为该疾病也可以通过使用IP受体拮抗剂治疗而得到缓解。
• Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
  申请人：Zhou Yuefen

  公开号：US20070197533A1

  公开（公告）日：2007-08-23

  The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammals, especially humans.

  本发明涉及抗菌性3,5-二氨基哌啶取代的芳香和杂环化合物及其制药组合物。本发明还涉及使用这些化合物治疗哺乳动物（尤其是人类）细菌感染的方法。
• Heterocyclic Benzoxazole Compositions as Inhibitors of Hepatitis C Virus
  申请人：Smith Paul

  公开号：US20120208856A1

  公开（公告）日：2012-08-16

  This invention relates to benzoxazole compounds, compositions and devices for delivering them, processes for manufacturing them, and methods of using them in the treatment of Hepatitis C Virus.

  本发明涉及苯并噁唑化合物、递送它们的组合物和装置、制造它们的过程，以及在治疗丙型肝炎病毒中使用它们的方法。